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H2O Solubility

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State

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LogP

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Dosage Forms

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Indication

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Pharmacology

Isosorbide Dinitrate is a moderate to long acting oral organic nitrate used for the relief and prophylactic management of angina pectoris. It relaxes the vascular smooth muscle and consequent dilatation of peripheral arteries and veins, especially the latter. Dilatation of the veins promotes peripheral pooling of blood and decreases venous return to the heart, thereby reducing left ventricular end- diastolic pressure and pulmonary capillary wedge pressure (preload). Arteriolar relaxation reduces systemic vascular resistance, systolic arterial pressure, and mean arterial pressure.

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Absorption

Absorption of isosorbide dinitrate after oral dosing is nearly complete, but bioavailability is highly variable (10% to 90%), with extensive first-pass metabolism in the liver. The average bioavailability of isosorbide dinitrate is about 25%.

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side effects and Toxicity

Symptoms of overdose include reduced cardiac output and hypotension.

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Patient Information

PATIENT INFORMATION

Patients should be told that the anti-anginal efficacy of isosorbide dinitrate is strongly related
to its dosing regimen, so the prescribed schedule of dosing should be followed carefully. In
particular, daily headaches sometimes accompany treatment with isosorbide dinitrate. In patients
who get these headaches, the headaches are a marker of the activity of the drug. Patients should
resist the temptation to avoid headaches by altering the schedule of their treatment with isosorbide
dinitrate, since loss of headache may be associated with simultaneous loss of anti-anginal efficacy.
Aspirin and/or acetaminophen, on the other hand, often successfully relieve isosorbide dinitrate-
induced headaches with no deleterious effect an isosorbide dinitrate's anti-anginal efficacy.

Treatment with isosorbide dinitrate may be associated with lightheadedness on standing, especially
just after rising from a recumbent or seated position. This effect may be more frequent in patients
who have also consumed alcohol